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LGK974

LGK974
LGK974 (NVP-LGK974) is an effective and selective PORCN inhibitor and inhibits Wnt signaling (IC50: 0.4 nM) in TM3 cells. It has been used in trials studying the treatment of Metastatic Colorectal Cancer and Squamous Cell Carcinoma, Head And Neck.
Catalog No. T2618Cas No. 1243244-14-5
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Purity:100%
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LGK974

Purity: 99.8%
Catalog No. T2618Alias WNT974, NVP-LGK974, LGK-974, LGK 974Cas No. 1243244-14-5

LGK974 (NVP-LGK974) is an effective and selective PORCN inhibitor and inhibits Wnt signaling (IC50: 0.4 nM) in TM3 cells. It has been used in trials studying the treatment of Metastatic Colorectal Cancer and Squamous Cell Carcinoma, Head And Neck.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$41In Stock
2 mg$59In Stock
5 mg$97In Stock
10 mg$167In Stock
25 mg$319In Stock
50 mg$573In Stock
100 mg$819In Stock
1 mL x 10 mM (in DMSO)$97In Stock
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Product Introduction

Bioactivity
Description
LGK974 (NVP-LGK974) is an effective and selective PORCN inhibitor and inhibits Wnt signaling (IC50: 0.4 nM) in TM3 cells. It has been used in trials studying the treatment of Metastatic Colorectal Cancer and Squamous Cell Carcinoma, Head And Neck.
Targets&IC50
Porcn:0.4 nM
In vitro
In both the MMTV-WNT1 mouse model of breast carcinoma and the human head and neck squamous cell carcinoma model (hn30), LGK-974 (3 mg/kg) inhibits the Wnt signaling pathway, leading to tumor regression without affecting mouse body weight. Additionally, LGK-974 (5 mg/kg, twice daily, orally) also suppresses the growth of RNF43-mutant pancreatic tumors (HPAF-II and Capan-2).
In vivo
LGK-974 inhibits a range of tested Wnts, with IC50 values between 0.05 to 2.4 nM. In the PORCN radioligand binding assay, LGK-974 effectively displaces [3H]GNF-1331 with an IC50 of 1 nM and exhibits minimal cytotoxicity at 20 μM. It specifically inhibits the growth of RNF43 mutant cell lines HPAF-II, PaTu 8988S, and Capan-2.
Kinase Assay
Radioligand binding assay: using the aforementioned membrane preps, filtration binding assays are performed. To reduce nonspecific binding, 96-well filtration plates are precoated as suggested by the manufacturer with 0.1% BSA and then washed four times with 0.1% BSA. Membrane preps (50 μg total protein) are incubated in polypropylene 96-well plates with 6.6 nM 3H-GNF-1331 in the presence or absence of a testing compound in binding buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 0.1% BSA) plus EDTA-free protease inhibitor mixture in a final volume of 150 μL for 3 h at room temperature. Binding reaction mixtures are then transferred to the precoated 96-well filtration plates, filtered, and washed using a 96-pin FilterMate Harvester. Radioactive signals are obtained using a Microplate Scintillation Counter TopCount. Curve fitting is performed using Prism[1].
Cell Research
Cells are plated in growth medium in a 96-well plate at a density of 6,000–12,000 cells per well and treated with DMSO or 1 μM LGK974. After 3 d, the cells are treated with fresh growth medium containing 20 μM EdU, which is included in the Click-iT EdU Alexa Fluor 488 HCS assay kit, and the plate was incubated for 2 h at 37 °C in a humidi?ed atmosphere containing 5% CO2. Cells are ?xed with ?nal 4% (mass/vol) paraformaldehyde for 30 min, washed with PBS, permeabilized, and stained with 50 μg/mL Hoechst in PBS for 30 min. After wash, the cells are proceeded to EdU detection according to the instruction of Click-iT EdU assay kit. Triplet wells are performed for each condition. (Only for Reference)
AliasWNT974, NVP-LGK974, LGK-974, LGK 974
Chemical Properties
Molecular Weight396.44
FormulaC23H20N6O
Cas No.1243244-14-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 73 mg/mL (184.1 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5224 mL12.6122 mL25.2245 mL126.1225 mL
5 mM0.5045 mL2.5224 mL5.0449 mL25.2245 mL
10 mM0.2522 mL1.2612 mL2.5224 mL12.6122 mL
20 mM0.1261 mL0.6306 mL1.2612 mL6.3061 mL
50 mM0.0504 mL0.2522 mL0.5045 mL2.5224 mL
100 mM0.0252 mL0.1261 mL0.2522 mL1.2612 mL

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